Bupranolol

Targets (3)

Identification

Name

Bupranolol

Accession Number

DB08808

Type

Small Molecule

Groups

Approved

Description

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to "propranolol":http://www.drugbank.ca/drugs/DB00571.

Pharmacology

Used to manage hypertension and tachycardia. Also used to treat glaucoma.

Structured Indications

Not Available

Pharmacodynamics

Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity.

Mechanism of action

Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

Quickly and completely absorbed from the gut with less than 10% oral bioavailability.

Volume of distribution

Not Available

Protein binding

76%

Metabolism

Over 90% undergo first-pass metabolism. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid, of which 88% are eliminated renally within 24 hours.